De Guidi G, Chillemi R, Costanzo L L, Giuffrida S, Sortino S, Condorelli G
Dipartimento di Scienze Chimiche, Università di Catania, Italy.
J Photochem Photobiol B. 1994 May;23(2-3):125-33. doi: 10.1016/1011-1344(94)06996-4.
Red blood cell lysis photosensitized by Suprofen (SPF) and the photolysis of the drug were investigated. The photohemolysis process occurs at a higher rate in anaerobic than aerobic conditions. The effect of additives demonstrates the involvement of free radicals and, to a lesser extent, singlet oxygen and hydroxyl radicals in the process. Photolysis of the drug at 310-390 nm in deaerated buffered solutions (pH 7.4) leads to a decarboxylation process with the formation of p-ethylphenyl 2-thienyl ketone (I), whereas in aerated solutions formation of photoproduct I and of the photoproducts p-acetylphenyl 2-thienyl ketone (II) and p-(1-hydroxyethyl)phenyl-2-thienyl ketone (III) occurs. The photodegradation products, which were separated and characterized, show a moderate lytic and photolytic activity. The rate of SPF photodegradation decreases in the presence of oxygen and increases in the presence of hydrogen donors. The overall results lead us to propose a mechanism of SPF photodegradation and a hemolysis scheme in which cell damage is provoked principally by the direct attack of drug radicals and secondarily by singlet oxygen and hydroxyl radicals.
研究了舒洛芬（SPF）光敏化的红细胞裂解以及该药物的光解作用。光溶血过程在厌氧条件下比需氧条件下以更高的速率发生。添加剂的作用表明自由基以及在较小程度上单线态氧和羟基自由基参与了该过程。在脱气缓冲溶液（pH 7.4）中，药物在310 - 390 nm处的光解导致脱羧过程，形成对乙基苯基2 - 噻吩基酮（I），而在通气溶液中会形成光产物I以及光产物对乙酰基苯基2 - 噻吩基酮（II）和对（1 - 羟乙基）苯基 - 2 - 噻吩基酮（III）。分离并表征的光降解产物显示出适度的裂解和光解活性。在有氧存在下，SPF的光降解速率降低，而在有氢供体存在下增加。总体结果使我们提出了SPF光降解的机制和溶血方案，其中细胞损伤主要由药物自由基的直接攻击引起，其次由单线态氧和羟基自由基引起。
